L-Threonine, N-acetyl-L-threonyl-(αR)-α-hydroxybenzenepropanoyl-2,3-didehydro-N-methylalanyl-L-alanyl-N-methyl-L-alanyl-(3R)-3-[[(2S,3R)-2-(acetylamino)-3-hydroxy-4-methyl-1-oxopentyl]oxy]-L-leucyl-N,O-dimethyl-, (7→1)-lactone
- CAS号:568580-02-9
- 英文名:L-Threonine, N-acetyl-L-threonyl-(αR)-α-hydroxybenzenepropanoyl-2,3-didehydro-N-methylalanyl-L-alanyl-N-methyl-L-alanyl-(3R)-3-[[(2S,3R)-2-(acetylamino)-3-hydroxy-4-methyl-1-oxopentyl]oxy]-L-leucyl-N,O-dimethyl-, (7→1)-lactone
- 中文名:L-Threonine, N-acetyl-L-threonyl-(αR)-α-hydroxybenzenepropanoyl-2,3-didehydro-N-methylalanyl-L-alanyl-N-methyl-L-alanyl-(3R)-3-[[(2S,3R)-2-(acetylamino)-3-hydroxy-4-methyl-1-oxopentyl]oxy]-L-leucyl-N,O-dimethyl-, (7→1)-lactone
- CBNumber:CB15490212
- 分子式:C46H69N7O15
- 分子量:960.09
- MOL File:568580-02-9.mol
- 沸点 :1232.4±65.0 °C(Predicted)
- 密度 :1.26±0.1 g/cm3(Predicted)
- 储存条件 :-20°C
- 溶解度 :Soluble in DMSO (up to 10 mg/ml)
- 形态 :lyophilized solid
- 酸度系数(pKa) :12.52±0.70(Predicted)
- 颜色 :White or off-white
- 稳定性 :Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
L-Threonine, N-acetyl-L-threonyl-(αR)-α-hydroxybenzenepropanoyl-2,3-didehydro-N-methylalanyl-L-alanyl-N-methyl-L-alanyl-(3R)-3-[[(2S,3R)-2-(acetylamino)-3-hydroxy-4-methyl-1-oxopentyl]oxy]-L-leucyl-N,O-dimethyl-, (7→1)-lactone性质、用途与生产工艺
- 生物活性 YM-254890 是一种从 Chromobacterium sp 中分离的选择性 Gαq/11 蛋白抑制剂。YM-254890 对其他 G 蛋白亚型无抑制作用。YM-254890 通过阻断 P2Y1 信号转导途径来抑制 ADP 诱导的血小板凝集,其 IC50 值低于 0.6 μM。
-
靶点
G αq/11 protein
-
体外研究
YM-254890 inhibits platelet aggregation induced by ADP (2, 5 and 20 μM) in human platelet-rich plasma with IC 50 values of 0.37, 0.39 and 0.51 μM. ADP mediates platelet aggregation via two G protein-coupled receptors, P2Y 1 and P2Y 12 . The effect of YM-254890 on the P2Y 1 and P2Y 12 signal transduction pathways using C6-15 cells stably expressing the human P2Y 1 or P2Y 12 receptors is examined. Stimulation of P2Y 1 -C6-15 cells by 2MeSADP leads to increases in intracellular calcium mobilization. In this assay, YM-254890 inhibits the increase in [Ca 2+ ] i with an IC 50 value of 0.031 μM. In contrast, 2MeSADP-induced inhibition of forskolin-stimulated adenylyl cyclase activity in P2Y 12 -C6-15 cells is unaffected by YM-254890 at 40 μM.
- 公司名称:BOC Sciences
- 联系电话:1-631-485-4226; 16314854226
- 电子邮件:info@bocsci.com
- 国家:美国
- 产品数:14059
- 优势度:65
- 公司名称:上海一飞生物科技有限公司
- 联系电话:021-65675885 18964387627
- 电子邮件:info@efebio.com
- 国家:中国
- 产品数:9806
- 优势度:58
- 公司名称:上海宏叶生物科技有限公司
- 联系电话:400-9205774
- 电子邮件:sales@glpbio.cn
- 国家:中国
- 产品数:6870
- 优势度:58
- 公司名称:TargetMol Chemicals Inc.
- 联系电话:+1-781-999-5354 +1-00000000000
- 电子邮件:marketing@targetmol.com
- 国家:美国
- 产品数:19892
- 优势度:58
- 公司名称:ChemeGen 中国
- 联系电话: 18818260767
- 电子邮件:sales@chemegen.com
- 国家:中国
- 产品数:11289
- 优势度:58
- 公司名称:上海麦克林生化科技股份有限公司
- 联系电话:021-50706066 15221275939
- 电子邮件:shenlinxing@macklin.cn
- 国家:中国
- 产品数:29802
- 优势度:58
- 公司名称:南京世洲生物科技有限公司
- 联系电话:025-85560043 15850508050
- 电子邮件:cindy.huang@synzest.com
- 国家:中国
- 产品数:12007
- 优势度:58